Therapeutic vegetable substances

ABSTRACT

A product containing papain, bromelain or mixtures thereof is intended for use as a medicinal product at a dosage of at least 5000 mg administered for at least one day in a single dose. This dosage relates to papain powder having a titre of 3 U/mg and bromelain powder having a titre of 2 U/mg, and to a patient with a body weight of 55 kg. In the case of variations of the titre and/or of the patient&#39;s weight, the dosage must be varied in proportion to said variations.

The present invention relates to the therapeutic use of vegetablesubstances, and in particular of papain, bromelain and mixtures thereof.

Vegetable papain consists of several proteolytic enzymes, whose specificaction is the hydrolysis of proteins, producing low molecular weightpeptides.

As it is known, the enzymes are catalysts that are extremely active inbiological reactions and belong to the chemical category of proteins,with chemical groups that can be of a non-protein nature (apoenzyme, theprotein part; coenzyme, the non-protein component, especially vitaminsand metals).

The enzymes have the character of specificity, and are named on thebasis of the substrate on which they act.

The active site of an enzyme consists of a group of amino acids, whichare not necessarily positioned in sequence on the polypeptide chain.

The amino acids are essential for human beings, as they make up thesequences of the proteins, as well as of non-protein peptides.

The amino acids are used by cells as nutrients, and are the basis offundamental physiological activities. They are molecules that contain aCOOH— group and an amino group NH₂—, joined to one and the same carbonatom C, the alpha carbon with respect to the carboxyl.

With respect to amino acids, the proteins are polymers of condensationof L,alpha amino acids, joined together in long chains by peptide bonds,with a number of proteins that can be extremely large, with L,alphaamino acids combined in various configurations: unknown, withpolypeptide chains of helical shape, with folding of the helices withparticipation of hydrogen bridges.

About 22 amino acids are present in the human body: 8 of these areconsidered essential, so defined because they are not produced by thehuman body, but are only obtained from the diet.

Vegetable papain can be considered to be derived from complexes of aminoacids with sequences characteristic of papain: lysine, threonine,valine, thionine, leucine, isoleucine, phenylalanine, histidine,arginine, oxyproline, aspartic acid, serine, glutamic acid, proline,alanine, cystine, tyrosine and others.

In the unripe, acidic fruit of Carica papaya there are 20 of the 22amino acids, including 7 of the 8 regarded as essential. Thephenylalanine contained in Carica papaya is among the precursors ofsubstances with antidepressant action. These elementary amino acids canthen naturally give rise to an enormous number of amino acid complexesof high molecular weight that are derived from individual amino acids byinteraction of various forces: van der Waals, dipole-dipoleinteractions, particularly hydrogen bonds, ionic bonds.

The aim of the present invention is to use the properties of papain andof bromelain appropriately for therapeutic purposes.

This aim is achieved with a product containing papain, bromelain ormixtures thereof for use as a medicinal product at a dosage of at least5000 mg administered for at least one day in a single dose, said dosagebeing referred respectively to papain powder having a titre of 3 U/mgand to bromelain powder having a titre of 2 U/mg, and to a patient witha body weight of 55 kg.

“Product containing papain, bromelain or mixtures thereof” means, in thepresent description, any product, in particular a drug, containing atleast one of the aforementioned compounds with any degree of purity ortitre and/or mixed with other substances.

It goes without saying that, in the case of variations of the titreand/or of the patient's weight, the dosage must be adjusted inproportion to said variations.

Advantageously, the papain is obtained from the unripe, sour, greenfruits of Carica papaya.

Vegetable papain has the following characteristics:

-   -   powder with titre of about 3 U/mg,    -   MW of about 23 000,

where 1 U corresponds to the amount of papain that hydrolyses 1micromole of N-alpha-benzoyl-L-arginine ethyl ester hydrochloride perminute at pH 6.2 at 25° C. Stable at 2-8° C.

The vegetable bromelain used (from pineapple) has the followingcharacteristics:

-   -   powder with titre of about 2 U/mg    -   MW of about 28 000,

where 1 U corresponds to the amount of bromelain that hydrolyses 1micromole of 4-nitrophenol per minute at pH 4.6 and 25° C. with thesubstrate N-alpha-carbobenzoyl-L-lysine-4-nitrophenyl ester.

The product with the dosage of the invention has a therapeutic effectagainst every form of benign and malignant tumour, both undergoingmetastasis, and with low or zero toxicity, and against other non-tumoraldiseases, with the warning to avoid the treatment of patients undergoingdialysis and women who are or are suspected of being pregnant.

Among the neoplastic diseases that are treatable, we may mention benignand malignant tumours of any kind, for example of the oral cavity,lymphoma, cerebrocerebellar neoplasias (ependymoma, medulloblastoma,gliomas), of the uterus, fibromas, of the breast, of the vertebralcolumn, of the intestine, of the colon and rectum, of the prostate,lung, gastric, of the liver, of the pancreas, of the gallbladder, of theoesophagus, of the stomach, of the bladder, of the kidney, bone,melanoma, of the ovaries and of the testes.

Among the non-tumoral diseases that are treatable we may mentionleukaemias, thyroid, multiple sclerosis, pneumonia, polyarthritis,osteomyelitis, diabetes mellitus, diseases of the circulatory system,diseases of the nervous system, infections of any nature, in particularpulmonary, varicoses, hepatic cirrhosis, leprosy, AIDS, autoimmunediseases, infarction, stroke, ALS and Parkinson's disease.

The product with the dosage of the present invention is usable not onlyin human beings, but also in animals, as well as concomitantly withother plant or animal enzymes, such as chymotrypsin, trypsin, pancreatinetc., and/or chemotherapeutic, herbal and dietetic agents and drugs,vegetable and synthetic active principles, and food supplements.

According to the invention, the daily dose of papain, bromelain andmixtures thereof is preferably at least 14000 mg, and even morepreferably is between 14000 and 20000 mg. For particularly weak ordebilitated patients, having for example low blood pressure or heartdisorders, the preferred daily dose is between 5000 and 7000 mg and isadministered for at least four consecutive days.

If necessary, administration of papain and bromelain can be combinedwith the administration of specific compounds, which avoid problemsconnected with the high single dose of administration ofpapain/bromelain per day (24 hours), and are at the same time able toactivate the cellular selectivity directed solely at infected cells andmetastases in progress.

These compounds—for example calcium chloride, potassium chloride, sodiumchloride, calcium sulphate, silica—can be energized beforehand byexposure to low-intensity magnetic fields and then stabilized.

These compounds in aqueous dilution or dispersion of 1 to 1000 can beadministered in amounts between 30 and 70% of that of papain andbromelain, in particular about 50%.

Treatment against carcinogenic cells is initiated with a single dose perday (24 hours), repeating it after 24 hours, then increasing it up tothe limit of tolerability of the healthy tissue or organ compared tothat which is carcinogenic.

After patients took a single daily dose of 14 000-20 000 milligrams ofpapain, values of blood pressure, degree of hydration and heart ratewere observed in the normal range, already with results that werepositive therapeutically.

It is also possible to administer adjuvant substances simultaneously,such as vitamin C, low doses of cortisone, plant complexes for energy,mineral salts, antiviral and antibacterial agents.

After a first single administration of 14 000-20 000 milligrams of purepapain in 24 hours, it is possible to extend the treatment for 7 dayswith 1500 mg of papain daily, then on alternate days for seven timeswith 1500 mg of papain administered per day, and, after a pause of oneweek, again on alternate days for seven times with 1500 mg of papainadministered per day.

The final result was excellent therapeutically. The values obtained20/30 days after completion of the whole therapy on subjects whopreviously had an approximate CEA value between 1000 and 2000, were CEA2 and CA125 1.5.

The patient receives a quick benefit immediately after beginningadministration of the product, even if the analytical test valuesdetermined with the current methods are subject to interference andtherefore the values are inaccurate during the administrations. It isnecessary to wait 20/30 days after the end of the administrations toobtain actual values.

The product according to the dosage of the present invention can also beapplied at an advanced stage of chemotherapy, radiotherapy, surgery etc.

It can be seen from the foregoing that the present patent descriptionprotects any therapy of every type of benign or malignant tumourundergoing metastasis, as well as of any type of non-cancerouspathology, even not mentioned.

The present patent description aims to protect the studies andexperiments conducted for several years about the use ofpapain/bromelain, pure or at varying degree of concentration—andoptionally with addition of synchronizing compounds, or mixed with otherplant or animal enzymes or plant or synthetic active principles, whetheror not antitumour, whether or not concomitantly with chemotherapeutic,herbal and dietetic agents and drugs—at a high daily dose neverpreviously investigated or patented, in the treatment of benign ormalignant tumours, of the diseases mentioned above and of any otherpathology not expressly mentioned, requiring therapeutic application ofhigh daily doses of papain/bromelain that were the subject of theaforementioned research and experiments.

The present patent description aims to protect the production,commercialization, sale to public or private health services orindividually of products based on more or less pure papain/bromelain ormixed with any other enzyme or pharmaceutical, chemical, herbal,dietetic product or plant or synthetic active principles, foodsupplements used at the high daily doses stated above according to thepresent patent, expressed in pure papain/bromelain or at theconcentration already stated above, or other concentration.

As already mentioned, the present invention also finds application inthe veterinary field, in parallel with all the applications mentionedabove for human beings.

The present patent description aims to protect the production,commercialization, and marketing of drugs, food supplements, herbalproducts, dietetic products, plant or chemical active principles, basedon vegetable papain/bromelain, pure or synchronized, or compounds basedon pure vegetable papain/bromelain mixed with other plant or animalenzymes already known for experimentation and commercialization (such aschymotrypsin, trypsin, pancreatin and others) with the intention andindication of using them at the high daily doses mentioned above in purepapain, or pure bromelain, or at various concentrations.

The present patent description aims to protect the research andexperimentation conducted into the therapeutic use of papain/bromelainat high daily dose, not previously patented or investigated, asvegetable papain/bromelain at the concentration specified above (or anyother vegetable papain/bromelain at varying concentration, referred tothe titre of that according to the present patent, taken daily), alsofor any type of non-cancerous pathology even not mentioned here.

“All things were made by Him, the Word, the Word of God” (John 1.1).

“Blessed Virgin Mary, Health of the Sick” (Pope Benedict XVI).

Naturally, without prejudice to the principle of the invention, thedetails of implementation and the embodiments can be varied widely fromwhat is described purely for purposes of illustration, while remainingwithin the scope of the invention as defined in the appended claims.

1-8. (canceled)
 9. Therapeutic method for treating tumour diseases,including providing for the administration of a product containingpapain, bromelain or mixtures thereof at a dosage of at least 5000 mgfor at least one day in a single dose, said dosage being referred to apapain powder, if present, having a titre of 3 U/mg and a bromelainpowder, if present, having a titre of 2 U/mg, and to a patient with abody weight of 55 kg, wherein in case of variations of the titre and/orthe patient's weight, the dosage must be adjusted in proportions to saidvariations.
 10. Method according to claim 9, wherein said dosage is atleast 14000 mg.
 11. Method according to claim 9, wherein said dosage isbetween 14000 and 20000 mg.